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Gastrin-releasing peptide (GRP) is a 27-amino acid neuropeptide and regulatory peptide hormone encoded by the *GRP* gene.[2][4][6] It is synthesized as a larger precursor (preproGRP) and processed to produce GRP and neuromedin C fragments.[4] GRP has significant physiological roles in the regulation of gastrointestinal and central nervous system functions, including stimulation of gastrin and other hormone release, promoting gastric acid secretion, influencing gastrointestinal motility, and stimulating cell proliferation.[3][4][6] Its main mechanism of action is through activation of the gastrin-releasing peptide receptor (GRPR, also known as BB2), a class A G protein-coupled receptor, which is the true therapeutic target in most drug development programs, especially for cancer and pruritus.[1][4] Elevated expression of the GRP/GRPR axis is implicated in several cancers, making pro-GRP and GRP themselves potential biomarkers for diagnosis or monitoring.[3][4]
Acts via binding and activating the gastrin-releasing peptide receptor (GRPR), a G protein-coupled receptor Induces intracellular signaling leading to hormone secretion and cell signaling events
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